Phosphoramidon Disodium Salt
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Phosphoramidon Disodium Salt是一种有效的金属蛋白酶抑制剂[1].
金属蛋白酶是有金属参与其催化机制的酶.多数金属蛋白酶需要锌,一些需要钴.
Phosphoramidon Disodium Salt是有效的金属蛋白酶抑制剂.在猪大动脉内皮细胞中,phosphoramidon(10-4 M)可抑制10-20%的免疫反应内皮素(IR-ET)释放,并能提高IR-CTF水平.这些结果表明phosphoramidon可通过影响大ET-1向ET-1的转化,减少IR-ET释放[1].在培养的内皮细胞中,phosphoramidon可抑制ET-1和大ET-1的C末端片段(CTF)的增加.然而,phosphoramidon可提高大ET-1分泌[2].
在麻醉大鼠中,phosphoramidon可抑制大ET-1的高血压效应[2].在小鼠中,phosphoramidon可通过抑制将大ET-1转化为ET-1的酶,抑制大ET-1诱导的致死性并提高血浆IR-ET-1[3].
参考文献:
[1]. Ikegawa R, Matsumura Y, Tsukahara Y, et al. Phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme. Biochem Biophys Res Commun, 1990, 171(2): 669-675.
[2]. Matsumura Y, Ikegawa R, Hisaki K, et al. Conversion of big endothelin-1 to endothelin-1 by phosphoramidon-sensitive metalloproteinase derived from aortic endothelial cells. J Cardiovasc Pharmacol, 1991, 17 Suppl 7: S65-7.
[3]. Matsuura A, Okumura H, Ashizawa N, et al. Big endothelin-1-induced sudden death is inhibited by phosphoramidon in mice. Life Sci, 1992, 50(21): 1631-1638.
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 587.47 |
Cas No. | 164204-38-0 |
Formula | C23H32N3Na2O10P |
Solubility | ≥58.7 mg/mL in DMSO; insoluble in EtOH; ≥52.5 mg/mL in H2O |
Chemical Name | sodium (S)-3-(1H-indol-3-yl)-2-((S)-4-methyl-2-((oxido(((2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)phosphoryl)amino)pentanamido)propanoate |
SDF | Download SDF |
Canonical SMILES | O=C([O-])[C@@H](NC([C@@H](NP(O[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O)([O-])=O)CC(C)C)=O)CC2=CNC3=C2C=CC=C3.[Na+].[Na+] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
从新鲜的猪胸主动脉分离的ECs |
溶解方法 |
在DMSO的溶解度>10mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
10- 7-10-4 M |
应用 |
在ECs (血管内皮细胞)中,phosphoramidon(10- 7-10-4 M)剂量依赖性地抑制膜部分的表观转化活性,并抑制膜部分诱导的大ET-1向ET-1(内皮素-1)的表观转化。ET-1是从ECs的培养基中分离的21个氨基酸多肽,通过加入phosphoramidon消除培养的EC中ET-1的分泌。 |
动物实验 [2]: | |
动物模型 |
野生型小鼠,NEP / NEP2缺陷小鼠 |
剂量 |
24μl (30 mM),每天一次,持续5天。 |
应用 |
Phosphoramidon的鼻内给药在野生型小鼠中能够显著升高大脑Aβ(β-淀粉样肽)的水平。在NEP / NEP2缺陷小鼠中,phosphoramidon显著提高Aβ水平。在缺乏NEP(Aβ降解酶)和NEP2的情况下,相对于Aβ1–42,phosphoramidon能显著提高Aβ1–40的水平,NEP和NEP2可能是啮齿动物脑中主要的“NEP样”Aβ1-42降解(phosphoramidon敏感的)酶。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Matsumura Y, Ikegawa R, Hisaki K., et al. Conversion of big endothelin-1 to endothelin-1 by phosphoramidon-sensitive metalloproteinase derived from aortic endothelial cells. J Cardiovasc Pharmacol, 1991, 17 Suppl 7: S65-7. [2] . Hanson LR., et al. Intranasal phosphoramidon increases beta-amyloid levels in wild-type and NEP/NEP2-deficient mice.J MolNeurosci. 2011 Mar;43(3):424-7. |
质量控制和MSDS
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